Solid forms of 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one as TOR kinase inhibitors

• US 9,981,971 B2
• Filed: 07/08/2016
• Issued: 05/29/2018
• Est. Priority Date: 04/16/2014
• Status: Active Grant

• Current Assignee: Signal Pharmaceuticals, LLC (Bristol-Myers Squibb Company)
• Original Assignee: Signal Pharmaceuticals, LLC (Bristol-Myers Squibb Company)
• Inventors: Boersen, Nathan
• Primary Examiner(s): Willis, Douglas M
• Application Number:
  US15/205,114
• Publication Number:
  US 20160318940A1
• Time in Patent Office: 690 Days
• Field of Search: 544350, 5462724, 5482664
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 37/02 Immunomodulators
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: C07D 487/04 Ortho-condensed systems

Abstract

Provided herein are formulations, processes, solid forms and methods of use relating to the Compound for formula 1:

having the name 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and tautomers thereof.

Claims

1. An amorphous form of the compound of formula (I):

2. The amorphous form of claim 1, which has a differential scanning calorimetry thermogram comprising an endotherm between 160°

C.±

5°

C. and 200°

C.±

5°

C. with a maximum at 188.1°

C.±

5°

C.

3. The amorphous form of claim 1, which has a glass transition temperature at 120°

C.±

5°

C.

4. The amorphous form of claim 1, which is pure.

5. A method for modulating target of rapamycin kinase activity in a subject, comprising administering to a subject in need thereof an effective amount of the amorphous form of claim 1.

6. The method of claim 5, wherein the subject suffers from a condition, disorder or disease selected from the group consisting of an inflammatory condition, an immunological condition, a cardiovascular condition, a neurological disorder, a neurodegenerative disease, an age-related disease, diabetes and obesity.